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JP4596751B2 - Anti-inflammatory analgesic patch - Google Patents

Anti-inflammatory analgesic patch Download PDF

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Publication number
JP4596751B2
JP4596751B2 JP2003166774A JP2003166774A JP4596751B2 JP 4596751 B2 JP4596751 B2 JP 4596751B2 JP 2003166774 A JP2003166774 A JP 2003166774A JP 2003166774 A JP2003166774 A JP 2003166774A JP 4596751 B2 JP4596751 B2 JP 4596751B2
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JP
Japan
Prior art keywords
weight
inflammatory analgesic
camphor
menthol
patch
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
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JP2003166774A
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Japanese (ja)
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JP2005002040A (en
Inventor
達也 小西
康子 阿部
裕治 町田
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Teikoku Seiyaku Co Ltd
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Teikoku Seiyaku Co Ltd
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Priority to JP2003166774A priority Critical patent/JP4596751B2/en
Application filed by Teikoku Seiyaku Co Ltd filed Critical Teikoku Seiyaku Co Ltd
Priority to EP04745727A priority patent/EP1632226A4/en
Priority to AU2004246924A priority patent/AU2004246924B2/en
Priority to KR1020057020411A priority patent/KR100946605B1/en
Priority to TW093116629A priority patent/TWI348383B/en
Priority to CNA2004800164330A priority patent/CN1805739A/en
Priority to CA2528649A priority patent/CA2528649C/en
Priority to US10/560,471 priority patent/US20070207088A1/en
Priority to PCT/JP2004/008097 priority patent/WO2004110428A1/en
Publication of JP2005002040A publication Critical patent/JP2005002040A/en
Application granted granted Critical
Publication of JP4596751B2 publication Critical patent/JP4596751B2/en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • A61K31/125—Camphor; Nuclear substituted derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/534—Mentha (mint)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/61—Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/81—Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7076—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising ingredients of undetermined constitution or reaction products thereof, e.g. rosin or other plant resins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Botany (AREA)
  • Dermatology (AREA)
  • Medical Informatics (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Biotechnology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Description

【０００１】
【発明の属する技術分野】
本発明は有効成分としてベンゾカインおよび反対刺激効果（Counter-irritation）を有する成分を含有する筋肉痛、関節痛、腰痛、肩こり、骨折痛などに用いる貼付剤に関し、さらに詳しくは、貼付時に不快感を与えるような刺激を軽減し、優れた効果を発現する消炎鎮痛貼付剤に関する。
【０００２】
【従来の技術】
従来から、有効成分としてｌ−メントール、ｄｌ−カンフル、サリチル酸メチル等を配合した薬剤含有粘着層を不織布、織布、ポリ塩化ビニルフィルム等の支持体に塗工し、薬剤含有粘着層の表面をポリプロピレンフィルム、ポリエチレンテレフタレートフィルム、紙等の剥離フィルムで被覆した消炎鎮痛貼付剤が種々市販されている。
【０００３】
また腰痛や肩こり等の慢性疾患に広く適用されている温感タイプの貼付剤として、前記した有効成分に加えて温感刺激成分であるトウガラシエキス、ノニル酸ワニリルアミド等を配合した貼付剤も多く市販されている。
【０００４】
これらの貼付剤中に配合されているｌ−メントール、ｄｌ−カンフル、サリチル酸メチル、トウガラシエキス、ノニル酸ワニリルアミド等は、いわゆる反対刺激効果を有する成分、いわゆる反対刺激薬として配合されているものである。
【０００５】
反対刺激効果を有する成分、いわゆる反対刺激薬とは、皮膚への局所的適用により、軽度の炎症を起こし、その結果、その皮膚の下にある組織の充血を消失させるために使用される薬剤であり、深部組織の炎症を軽減する目的で、皮膚を刺激したり、軽度の炎症を生じさせたりする薬剤である。
【０００６】
しかしながら、この反対刺激薬は、適用症状によっては、有効成分であるｌ−メントール、サリチル酸メチル等の刺激により患部に痛みを感じたり、かぶれが生じたりすることがある。さらに、温感刺激成分を配合した貼付剤では年齢、性差、貼付部位により、温感の度合いがかなり異なるものであって、発赤、かぶれ等不快な皮膚刺激症状を起こすという問題がある。また貼付剤の剥離後も刺激が残り、例えば入浴時に激しい痛みを感じることも経験されている。
【０００７】
このような刺激、痛みを軽減させるために、種々の生薬成分を配合し、刺激を緩和する試みがなされているが、いまだ充分な効果は得られておらず、更なる改良品の開発が求められているのが現状である。
【０００８】
【発明が解決しようとする課題】
本発明は、上記の現状に鑑み、優れた消炎鎮痛効果を発揮すると共に、貼付時の不快な刺激感を軽減した、消炎鎮痛貼付剤を提供することを課題とする。
【０００９】
かかる課題を解決するべく、本発明者らは皮膚刺激緩和について鋭意検討した結果、有効成分としてベンゾカインを配合し、それと共に反対刺激効果を有する成分を、その効果が期待できる量配合した貼付剤が、不快な刺激感を軽減するものであり、また、消炎鎮痛として期待される効果を充分に発揮し得るものであることを見出し、本発明を完成させるに至った。
【００１０】
【課題を解決するための手段】
したがって本発明は、その基本的態様として、有効成分としてベンゾカインおよび反対刺激効果（Counter-irritation）を有する成分を配合してなることを特徴とする消炎鎮痛貼付剤である。
【００１１】
具体的には、本発明はベンゾカインをその有効量として、０．５〜２０重量％含有する消炎鎮痛貼付剤である。
【００１２】
また、より具体的な本発明は、ベンゾカインと共に、ｌ−メントール、ｄｌ−メントール、ｄｌ−カンフル、ｄ−カンフル、サリチル酸メチル、サリチル酸グリコール、ハッカ油、ユーカリ油、カプサイシン、トウガラシ抽出物、ノニル酸ワニリルアミドからなる群から選択される一種または二種以上の反対刺激効果を有する成分を配合した消炎鎮痛貼付剤である。
【００１３】
すなわち本発明の消炎鎮痛貼付剤は、ベンゾカインをその有効量配合すると共に、反対刺激効果を有する成分を、その効果が期待できる量配合した点に特徴を有するものである。
【００１４】
したがって、より具体的な本発明の貼付剤にあっては、反対刺激効果を有する成分の配合量が、ｌ−メントール、ｄｌ−メントール、ｄｌ−カンフル、ｄ−カンフル、サリチル酸メチル、サリチル酸グリコール、ハッカ油またはユーカリ油にあっては０．０１〜３０重量％であり、カプサイシン、トウガラシ抽出物またはノニル酸ワニリルアミドにあっては０．００１〜５重量％である消炎鎮痛貼付剤である。
【００１５】
さらに具体的態様に基づく本発明は、貼付剤としての剤型が水分を１０〜８０重量％含有する水性パップ剤である消炎鎮痛貼付剤であり、詳細には、水分を１０〜８０重量％含有する水性パップ膏体中に、ベンゾカインを０．５〜２０重量％配合し、さらにｌ−メントール、ｄｌ−メントール、ｄｌ−カンフル、ｄ−カンフル、サリチル酸メチル、サリチル酸グリコール、ハッカ油、ユーカリ油、カプサイシン、トウガラシ抽出物、ノニル酸ワニリルアミドからなる群から選択される反対刺激効果を有する成分を一種または二種以上配合したことを特徴とする消炎鎮痛貼付剤である。
【００１６】
また本発明は、別の態様として、消炎鎮痛貼付剤の有効成分として含有される反対刺激効果を有する成分が有する皮膚刺激感を緩和するためにベンゾカインを併用する、ベンゾカインの使用方法でもある。
【００１７】
【発明の実施の形態】
以下、本発明につき詳しく説明する。
本発明が提供する消炎鎮痛貼付剤は、有効成分としてベンゾカインおよび反対刺激効果を有する成分を併用配合し、貼付時の皮膚刺激感を緩和させると共に、優れた消炎鎮痛効果を発揮することを特徴とする。
【００１８】
かかる目的のために使用されるベンゾカインの配合量は、製剤中０．５〜２０重量％が好ましく、より好ましくは５〜１５重量％である。ベンゾカインの配合量が０．５重量％未満であると充分な消炎鎮痛効果を得ることができず、また２０重量％を越えて配合すると製剤の安定性が得られなくなり、好ましいものではない。
【００１９】
一方、本発明の貼付剤においてベンゾカインと共に配合される反対刺激効果を有する成分としては、ｌ−メントール、ｄｌ−メントール、ｄｌ−カンフル、ｄ−カンフル、サリチル酸メチル、サリチル酸グリコール、ハッカ油、ユーカリ油、カプサイシン、トウガラシ抽出物、ノニル酸ワニリルアミドをあげることができ、これらの成分の一種または二種以上を使用することができる。
【００２０】
これらの反対刺激効果を有する成分の配合量は、消炎鎮痛貼付剤において通常に配合される量で良く、具体的には、ｌ−メントール、ｄｌ−メントール、ｄｌ−カンフル、ｄ−カンフル、サリチル酸メチル、サリチル酸グリコール、ハッカ油、ユーカリ油にあっては製剤中０．０１〜３０重量％が好ましく、より好ましくは０．１〜１５重量％である。また、カプサイシン、トウガラシ抽出物、ノニル酸ワニリルアミドにあっては製剤中０．００１〜５重量％が好ましく、より好ましくは０．００５〜３重量％である。
【００２１】
上記の配合量未満であると、貼付剤としてこれら成分の有する反対刺激効果を発揮することができず、また上記配合量を超える場合には、皮膚刺激が強い貼付剤となり、好ましいものではない。
【００２２】
本発明が提供する消炎鎮痛貼付剤には、上記成分に加え、外用製剤に通常に配合される種々の成分を配合することができる。そのような成分としては、具体的には、血行促進作用のある酢酸トコフェロール等のビタミンＥ類、ニコチン酸アミド、ニコチン酸ベンジル等、鎮痛消炎作用のあるグリチルレチン、グリチルリチン酸、グリチルリチン酸ジカリウム等、抗アレルギー作用を有するジフェンヒドラミン、マレイン酸クロルフェニラミン等、さらにはアルニカチンキ、オウバクエキス、カミツレエキス、サンシシエキス、サンショウエキス、シコンエキス、セイヨウトチノミエキス、センブリエキス等の植物抽出物、防腐剤としてパラオキシ安息香酸メチル、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、パラオキシ安息香酸ブチル等のパラベン類、フェノキシエタノール、安息香酸、サリチル酸、塩化ベンゼトニウム、塩化セチルピリジニウム、塩酸クロルヘキシジン等、酸化防止剤としてブチルヒドロキシアニソール、ジブチルヒドロキシトルエン、アスコルビン酸、アスコルビン酸ナトリウム等をあげることができる。
【００２３】
本発明が提供する消炎鎮痛貼付剤の剤型としては、パップ剤、プラスター剤、テープ剤等が挙げられ、その基剤として用いられる成分は、従来から貼付剤基剤として一般的に使用されているものを用いることができる。
【００２４】
具体的には、例えば水溶性パップ剤においてはゼラチン、プルラン、ポリビニルピロリドン、ポリビニルアルコール、メチルセルロース、エチルセルロース、カルボキシメチルセルロース、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、ポリアクリル酸、ポリアクリル酸ナトリウム、アクリル酸共重合体、無水マレイン酸共重合体、デンプン・アクリル酸ナトリウムグラフト重合体、カルボキシビニルポリマー、アルギン酸ナトリウム、キサンタンガム、カンテン、カラギーナン等の一種または二種以上の水溶性高分子物質が配合される。その配合量は、基剤の強度および冷却の設定能、または製造時の作業性等により異なるが、通常、膏体全重量に対して３〜４０重量％である。
【００２５】
かかる水溶性高分子物質からなる水性パップ剤の基剤成分を架橋する場合には、カリウムミョウバン、アルミニウムミョウバン、塩化マグネシウム、塩化カルシウム、塩化アルミニウム、水酸化アルミニウム、水酸化カルシウム、水酸化第二鉄、リン酸カルシウム、クエン酸カルシウム、アルミニウムグリシネート、メタケイ酸アルミン酸マグネシウム、ケイ酸アルミン酸マグネシウム、メタケイ酸アルミニウム、ケイ酸マグネシウム、合成ヒドロタルサイト等の多価金属、あるいはポリエチレングリコールジグリシジルエーテル、エチレングリコールジグリシジルエーテル、グリセリンジグリシジルエーテル、トリグリセリンジグリシジルエーテル等の架橋剤が用いられ、これら架橋剤の配合量は膏体全重量に対し０．００１〜５重量％が好ましく、より好ましくは０．００５〜３重量％である。
これらの架橋剤は、一種単独でまたは２種以上を適宜組み合わせて使用することができる。
【００２６】
上記の架橋剤を用いる場合には、架橋調整剤を配合することが好ましい。そのような架橋調整剤としては、クエン酸、リンゴ酸、酒石酸、グリコール酸、フマル酸、コハク酸、エデト酸等の有機酸またはその塩類などが用いられ、これら架橋調整剤は、一種単独または二種以上を適宜組み合わせて、使用することができる。
【００２７】
さらに、基剤中にはカオリン、ベントナイト、酸化チタンなどの無機塩および通常の吸収助剤として用いられるヒマシ油、クロタミトン、ミリスチン酸イソプロピル、アジピン酸イソプロピル、セバシン酸ジイソプロピル、ジイソプロパノールアミン、Ｎ，Ｎ−ジエチル−ｍ−トルアミド等を配合することができ、その配合量としては膏体重量に対して０．０１〜２０重量％、好ましくは０．１〜１０重量％である。またエチレングリコール、ジエチレングリコール、ポリエチレングリコール、プロピレングリコール、ポリプロピレングリコール、１，３−ブチレングリコール、グリセリン、ソルビトールなどの多価アルコールを配合することができる。多価アルコールを配合する場合、膏体全重量に対し好ましくは３〜６０重量％、より好ましくは１０〜５０重量％である。
【００２８】
本発明が提供する消炎鎮痛貼付剤において、その一態様である水性パップ剤にあっては水分を含有するものであり、その水分含量は膏体全重量に対して１０〜８０重量％とするのがよく、より好ましくは３０〜７５重量％である。
【００２９】
また、上記水性パップ剤の膏体のｐＨは、３．０〜９．０に調整されるのが良く、好ましくは３．５〜８、より好ましくは４〜７．５とするのがよい。ｐＨが３．０未満では酸性が強すぎることにより皮膚刺激が発生し、また９．０を越えた場合には皮膚の腐食損傷等不都合な作用が発生するため好ましくない。
【００３０】
上記の水性パップ剤の支持体としては不織布、織布、またはこれらとポリエチレン、ポリプロピレン、ポリ塩化ビニル、ポリ塩化ビニリデン、ポリウレタン、ポリエチレンテレフタレートとのラミネート物等が使用される。これらの中でも不織布が特に好ましく、不織布としてはナイロン、ビニリデン、ポリ塩化ビニル、ポリエステル、アクリル、ポリエチレン、ポリプロピレン、ポリウレタン等の化学繊維、綿、羊毛、麻、絹等の天然繊維から選ばれる少なくとも一種の繊維からなる不織布が好適である。
【００３１】
また、本発明が提供する消炎鎮痛貼付剤における別の態様であるプラスター剤にあっては、スチレン−イソプレン−スチレンブロックコポリマー等の合成ゴム系粘着剤、天然ゴム系粘着剤、水素添加石油樹脂、ロジン、水素添加ロジン、ポリビニルアルコール、ポリビニルピロリドンなどよりなる粘着剤を使用することができ、この粘着剤の配合量は膏体全重量に対し１５〜８０重量％とすることができる。
【００３２】
更に、上記のプラスター剤においてはポリブデン、ポリイソブチレン等の液状ゴム、流動パラフィン、植物油、ラノリン等の軟化剤を配合することもでき、この軟化剤の配合量は、膏体全重量に対し１０〜４０重量％とすることができる。また上記のプラスター剤には、必要に応じて脂肪酸エステル類、高級アルコール等の経皮吸収促進剤や前述の外用製剤に通常に配合される成分を配合することもできる。
【００３３】
上記のプラスター剤の支持体としては、セルロース誘導体フィルム、ポリエチレンテレフタレートフィルム、ナイロンフィルム、ポリ塩化ビニルフィルム、ポリエチレンフィルム、ポリウレタンフィルム、ポリ塩化ビニリデンフィルム等の樹脂フィルムやアルミニウムなどの金属シート、不織布、織布等が用いられ、樹脂フィルム、金属シートは単独または不織布等と積層して用いることができる。
【００３４】
本発明が提供する消炎鎮痛貼付剤の製造は、例えば、水性パップ剤にあっては、ベンゾカイン、反対刺激効果を有する成分さらには所望により種々の成分をよく混合し、例えばペースト状に調製した後、これを紙、織布、不織布、プラスチックフィルム等の支持体（基材）上に所望の厚さで塗付・積層し、さらにこれに透明の保護フィルム、例えば、ポリエチレンフィルムを被覆し、所望の大きさに裁断することにより製造することができる。薬物含有膏体層として基材シート上に積層させる層の重量は一概に限定し得ないが、塗布量として２００〜２０００ｇ／ｍ２、好ましくは４００〜１５００ｇ／ｍ２であれば十分である。
【００３５】
また、プラスター剤にあっては、例えばスチレン−イソプレン−スチレンブロックコポリマー等の合成ゴム系粘着剤、軟化剤、粘着付与剤、抗酸化剤および充填剤等を溶融練合し、これにベンゾカイン、反対刺激効果を有する成分さらには所望により種々の成分を加え均一に練合した後、支持体フィルム上に展延し、適当な大きさと形状に切断することにより製造することができる。
【実施例】
以下に、実施例および比較例を示すことにより、本発明の消炎鎮痛貼付剤を具体的に説明するが、本発明はこれらに限定されるものではない。
【００３６】
実施例１〜３：水性パップ剤
下記表１に示す組成の水性パップ基剤を常法に従って調製し、これを不織布上に均一の厚さに塗工し、更にその表面をポリエチレンテレフタレートフィルムで覆い、実施例１〜３の水性パップ剤を得た。
【００３７】
【表１】
表１：実施例処方例

Figure 0004596751
【００３８】
比較例１〜３：
下記表２に示す組成（ベンゾカインを含まない）の水性パップ基剤を常法に従って調製し、これを不織布上に均一の厚さに塗工し、更にその表面をポリエチレンテレフタレートフィルムで覆い、比較例１〜３の水性パップ剤を得た。
【００３９】
【表２】
表２：比較例処方例
Figure 0004596751
【００４０】
実施例４：プラスター剤
下記に示す処方に従って、スチレン・イソプレン・スチレンブロック共重合体、脂環族飽和炭化水素樹脂、合成ゴムおよびジブチルヒドロキシトルエンを溶融練合し、ノニル酸ワニリルアミド、サリチル酸メチル、ｄｌ−カンフル、ベンゾカインを加えて均一に練合した後、支持体フィルム上に展延し、プラスター剤を得た。
【００４１】
処方：
ノニル酸ワニリルアミド ０．０１重量％
サリチル酸メチル ５．０重量％
ｄｌ−カンフル ２．０重量％
ベンゾカイン ５．０重量％
スチレン・イソプレン・スチレン
ブロック共重合体 ２２．０重量％
脂環族飽和炭化水素樹脂 ４６．９９重量％
合成ゴム １８．０重量％
ジブチルヒドロキシトルエン １．０重量％
【００４２】
試験例１：
実施例１〜３、比較例１〜３の水性パップ剤および実施例４のプラスター剤について、被験者２０名の上腕部内側に貼付し、貼付後１０、２０、３０、６０および９０分後の刺激の強さについて、官能試験により評価した。
刺激の評価基準は、以下の５段階に分け、被験者１０名の平均値で示した。
４：痛みが強い
３：刺激の他に痛みを感じる
２：適度な刺激を感じる
１：弱い刺激を感じる
０：刺激を感じない
その結果を表３に示した。
【００４３】
【表３】
表３：刺激感試験結果
Figure 0004596751
【００４４】
上記の表３中に示した結果からも判明するように、本発明の貼付剤（実施例１〜４）は、貼付後２０分程度で適度な刺激が発現し、比較例に比べ３０〜９０分の貼付時間においては刺激に対する痛みを感じることが少なく、適度な刺激が持続しているものであった。
【００４５】
試験例２：
実施例１および比較例１の貼付剤を、関節痛の症状を持つ社内ボランティア１０名（医師の監視下のもと、インフォームドコンセントを得て実施）に使用し、その効果を評価した。
評価基準は次の通りである。
＋＋：痛みが軽減し楽になった
＋：痛みが少し軽減した
±：変わらない
−：痛みが増した
その結果を表４に示した。
【００４６】
【表４】
表４：効果試験結果
Figure 0004596751
【００４７】
試験例３：
実施例３および比較例３の貼付剤を、腰痛の症状を持つ社内ボランティア１０名（医師の監視下のもと、インフォームドコンセントを得て実施）に使用し、その効果を評価した。
評価基準は次の通りである。
＋＋：痛みが軽減し楽になった
＋：痛みが少し軽減した
±：変わらない
−：痛みが増した
その結果を表５に示した。
【００４８】
【表５】
表５：効果試験結果
Figure 0004596751
【００４９】
上記の表４および５に示した結果からも判明するように、本発明の貼付剤は、比較例の貼付剤に比べ、関節痛または腰痛の症状に対して、その有効率が高いものであった。
【００５０】
【発明の効果】
以上記載のように、本発明の貼付剤は、有効成分としてベンゾカインと共に反対刺激効果（Counter-irritation）を有する成分を配合したものであり、従来の反対刺激効果を有する成分を配合した製剤に比べ、皮膚刺激緩和効果を有し、そのうえ、期待される消炎鎮痛効果を充分に発揮するものである。
したがってその医療上の効果は多大なものである。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a patch for muscular pain, joint pain, low back pain, stiff shoulder, fracture pain, etc. containing benzocaine as an active ingredient and a component having counter-irritation effect. The present invention relates to an anti-inflammatory analgesic patch which reduces irritation and gives an excellent effect.
[0002]
[Prior art]
Conventionally, a drug-containing adhesive layer containing l-menthol, dl-camphor, methyl salicylate, etc. as an active ingredient is applied to a support such as a nonwoven fabric, a woven fabric, or a polyvinyl chloride film, and the surface of the drug-containing adhesive layer is applied. Various anti-inflammatory analgesic patches coated with a release film such as a polypropylene film, a polyethylene terephthalate film or paper are commercially available.
[0003]
In addition, as a warm-type patch widely applied to chronic diseases such as low back pain and shoulder stiffness, many patches are also commercially available that contain hot pepper stimulating ingredients such as pepper extract and nonyl acid vanillylamide in addition to the above-mentioned active ingredients. Has been.
[0004]
L-Menthol, dl-camphor, methyl salicylate, pepper extract, nonylic acid vanillylamide, etc. blended in these patches are blended as so-called counter-stimulating agents, so-called counter-stimulating agents. .
[0005]
A counter-irritant ingredient, a so-called counter-stimulant, is a drug that is used to cause mild irritation by topical application to the skin and, as a result, eliminate the hyperemia of the tissue under the skin. It is a drug that stimulates the skin and causes mild inflammation for the purpose of reducing inflammation in deep tissues.
[0006]
However, this counterstimulant may cause pain or irritation to the affected area due to stimulation of 1-menthol or methyl salicylate, which are active ingredients, depending on the symptoms of application. Furthermore, the patch containing a warming sensation component has a different degree of warmth depending on the age, sex difference, and application site, and has the problem of causing unpleasant skin irritation such as redness and rash. It has also been experienced that irritation remains after the patch is peeled off, and that, for example, severe pain is felt during bathing.
[0007]
In order to alleviate such irritation and pain, various herbal medicine ingredients have been blended and attempts have been made to alleviate the irritation, but sufficient effects have not yet been obtained, and further improvements need to be developed. This is the current situation.
[0008]
[Problems to be solved by the invention]
In view of the above-mentioned present situation, an object of the present invention is to provide an anti-inflammatory analgesic patch that exhibits an excellent anti-inflammatory analgesic effect and reduces an unpleasant irritation at the time of application.
[0009]
In order to solve such problems, the present inventors have intensively studied about the reduction of skin irritation. As a result, a patch containing benzocaine as an active ingredient and an ingredient having an anti-irritant effect in an amount that can be expected to have the effect is obtained. The present invention has been found to reduce unpleasant irritation and to fully exhibit the effects expected as anti-inflammatory analgesia.
[0010]
[Means for Solving the Problems]
Therefore, the present invention is an anti-inflammatory analgesic patch characterized by comprising, as its basic aspect, benzocaine as an active ingredient and a component having counter-irritation effect (Counter-irritation).
[0011]
Specifically, the present invention is an anti-inflammatory analgesic patch containing 0.5 to 20% by weight of benzocaine as its effective amount.
[0012]
Further, the present invention more specifically includes benzocaine, l-menthol, dl-menthol, dl-camphor, d-camphor, methyl salicylate, glycol salicylate, peppermint oil, eucalyptus oil, capsaicin, capsicum extract, nonyl acid vanillylamide An anti-inflammatory analgesic patch containing one or more components having a counterstimulating effect selected from the group consisting of:
[0013]
That is, the anti-inflammatory analgesic patch of the present invention is characterized in that benzocaine is blended in an effective amount and a component having a counter-stimulating effect is blended in an amount where the effect can be expected.
[0014]
Therefore, in the more specific patch of the present invention, the compounding amount of the component having the counter stimulating effect is 1-menthol, dl-menthol, dl-camphor, d-camphor, methyl salicylate, glycol salicylate, mint. The anti-inflammatory analgesic patch is 0.01 to 30% by weight for oil or eucalyptus oil, and 0.001 to 5% by weight for capsaicin, pepper extract or nonylic acid vanillylamide.
[0015]
Furthermore, the present invention based on a specific embodiment is an anti-inflammatory analgesic patch, which is an aqueous patch containing 10 to 80% by weight of water as a patch, and specifically contains 10 to 80% by weight of water. 0.5 to 20% by weight of benzocaine in an aqueous paste, and further l-menthol, dl-menthol, dl-camphor, d-camphor, methyl salicylate, glycol salicylate, mint oil, eucalyptus oil, capsaicin An anti-inflammatory analgesic patch comprising one or more components having an anti-irritant effect selected from the group consisting of pepper extract and nonylic acid vanillylamide.
[0016]
Moreover, this invention is also the usage method of a benzocaine which uses benzocaine together in order to relieve the skin irritation which the component which has the opposite irritation effect contained as an active ingredient of an anti-inflammatory analgesic patch has another aspect.
[0017]
DETAILED DESCRIPTION OF THE INVENTION
Hereinafter, the present invention will be described in detail.
The anti-inflammatory analgesic patch provided by the present invention is characterized by combining benzocaine and an ingredient having an anti-irritant effect as an active ingredient, relieving skin irritation at the time of application, and exhibiting an excellent anti-inflammatory analgesic effect. To do.
[0018]
The blending amount of benzocaine used for this purpose is preferably 0.5 to 20% by weight, more preferably 5 to 15% by weight in the preparation. If the amount of benzocaine is less than 0.5% by weight, a sufficient anti-inflammatory analgesic effect cannot be obtained, and if it exceeds 20% by weight, the stability of the preparation cannot be obtained, which is not preferable.
[0019]
On the other hand, as a component having a counterstimulating effect blended with benzocaine in the patch of the present invention, 1-menthol, dl-menthol, dl-camphor, d-camphor, methyl salicylate, glycol salicylate, mint oil, eucalyptus oil, Capsaicin, pepper extract, nonylic acid vanillylamide can be mentioned, and one or more of these components can be used.
[0020]
The amount of these components having an anti-irritant effect may be an amount usually blended in anti-inflammatory analgesic patches, specifically, 1-menthol, dl-menthol, dl-camphor, d-camphor, methyl salicylate. , Salicylic acid glycol, peppermint oil, eucalyptus oil, 0.01 to 30% by weight in the preparation is preferable, more preferably 0.1 to 15% by weight. Moreover, in capsaicin, a red pepper extract, and nonyl acid vanillylamide, 0.001 to 5 weight% is preferable in a formulation, More preferably, it is 0.005 to 3 weight%.
[0021]
If the blending amount is less than the above-mentioned amount, the counter-irritant effect of these components cannot be exhibited as a patch, and if the blending amount exceeds the above-mentioned amount, the skin irritation is strong, which is not preferable.
[0022]
The anti-inflammatory analgesic patch provided by the present invention may contain various components that are usually blended in external preparations in addition to the above components. Specific examples of such components include vitamin E such as tocopherol acetate having a blood circulation promoting action, nicotinic acid amide, benzyl nicotinate and the like, glycyrrhetin having analgesic / anti-inflammatory action, glycyrrhizic acid, dipotassium glycyrrhizate and the like. Diphenhydramine with allergic action, chlorpheniramine maleate, etc., as well as plant extracts such as arnica tincture, agaric extract, chamomile extract, sanshi extract, salamander extract, coconut extract, horse chestnut extract, assembly extract, paraoxybenzoic acid as an antiseptic Parabens such as methyl, ethyl paraoxybenzoate, propyl paraoxybenzoate, butyl paraoxybenzoate, phenoxyethanol, benzoic acid, salicylic acid, benzethonium chloride, cetylpyridinium chloride, Chlorhexidine or the like, butylhydroxyanisole as antioxidants, dibutylhydroxytoluene, ascorbic acid, may be mentioned sodium ascorbate and the like.
[0023]
Examples of the dosage form of the anti-inflammatory analgesic patch provided by the present invention include poultices, plasters, tapes and the like, and the components used as the base have been conventionally used as patch bases. Can be used.
[0024]
Specifically, for example, in a water-soluble cataplasm, gelatin, pullulan, polyvinylpyrrolidone, polyvinyl alcohol, methylcellulose, ethylcellulose, carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, polyacrylic acid, sodium polyacrylate, acrylic acid copolymer , Maleic anhydride copolymer, starch / sodium acrylate graft polymer, carboxyvinyl polymer, sodium alginate, xanthan gum, agar, carrageenan and the like, or two or more water-soluble polymer substances are blended. The blending amount varies depending on the strength of the base and the ability to set cooling, or workability during production, but is usually 3 to 40% by weight based on the total weight of the paste.
[0025]
When cross-linking the base component of an aqueous cataplasm composed of such a water-soluble polymer substance, potassium alum, aluminum alum, magnesium chloride, calcium chloride, aluminum chloride, aluminum hydroxide, calcium hydroxide, ferric hydroxide , Calcium phosphate, calcium citrate, aluminum glycinate, magnesium aluminate metasilicate, magnesium aluminate silicate, aluminum metasilicate, magnesium silicate, synthetic hydrotalcite and other polyvalent metals, or polyethylene glycol diglycidyl ether, ethylene glycol Crosslinking agents such as diglycidyl ether, glycerin diglycidyl ether, and triglycerin diglycidyl ether are used, and the blending amount of these crosslinking agents is 0.001 to 5% by weight based on the total weight of the plaster. Preferred, more preferably from 0.005 to 3 wt%.
These crosslinking agents can be used singly or in appropriate combination of two or more.
[0026]
When using the above-mentioned crosslinking agent, it is preferable to incorporate a crosslinking regulator. As such a crosslinking regulator, an organic acid such as citric acid, malic acid, tartaric acid, glycolic acid, fumaric acid, succinic acid, edetic acid, or a salt thereof is used. Two or more species can be used in appropriate combination.
[0027]
Furthermore, the base contains inorganic salts such as kaolin, bentonite, titanium oxide, and castor oil, crotamiton, isopropyl myristate, isopropyl adipate, diisopropyl sebacate, diisopropanolamine, N, N, which are commonly used as absorption aids. -Diethyl-m-toluamide etc. can be mix | blended, As the compounding quantity, it is 0.01-20 weight% with respect to the plaster weight, Preferably it is 0.1-10 weight%. In addition, polyhydric alcohols such as ethylene glycol, diethylene glycol, polyethylene glycol, propylene glycol, polypropylene glycol, 1,3-butylene glycol, glycerin and sorbitol can be blended. When blending polyhydric alcohol, it is preferably 3 to 60% by weight, more preferably 10 to 50% by weight, based on the total weight of the plaster.
[0028]
In the anti-inflammatory analgesic patch provided by the present invention, the aqueous poultice that is one embodiment thereof contains water, and the water content is 10 to 80% by weight with respect to the total weight of the paste. More preferably, it is 30 to 75% by weight.
[0029]
The pH of the paste for the aqueous cataplasm is preferably adjusted to 3.0 to 9.0, preferably 3.5 to 8, and more preferably 4 to 7.5. If the pH is less than 3.0, skin irritation occurs due to too strong acidity, and if it exceeds 9.0, adverse effects such as corrosion damage to the skin occur.
[0030]
As the support for the aqueous cataplasm, non-woven fabric, woven fabric, or a laminate of these with polyethylene, polypropylene, polyvinyl chloride, polyvinylidene chloride, polyurethane, polyethylene terephthalate, or the like is used. Among these, non-woven fabrics are particularly preferred, and the non-woven fabric is at least one selected from chemical fibers such as nylon, vinylidene, polyvinyl chloride, polyester, acrylic, polyethylene, polypropylene, polyurethane, and natural fibers such as cotton, wool, hemp, silk, etc. Nonwoven fabrics made of fibers are preferred.
[0031]
Further, in the plaster agent which is another aspect in the anti-inflammatory analgesic patch provided by the present invention, a synthetic rubber adhesive such as styrene-isoprene-styrene block copolymer, natural rubber adhesive, hydrogenated petroleum resin, A pressure-sensitive adhesive made of rosin, hydrogenated rosin, polyvinyl alcohol, polyvinylpyrrolidone, or the like can be used. The amount of the pressure-sensitive adhesive can be 15 to 80% by weight based on the total weight of the plaster.
[0032]
Furthermore, in the above plaster agent, a soft rubber such as liquid rubber such as polybutene and polyisobutylene, liquid paraffin, vegetable oil, and lanolin can be blended, and the blending amount of the softener is 10 to 10% of the total weight of the plaster. It can be 40% by weight. In addition, the above-mentioned plaster agent can be blended with percutaneous absorption accelerators such as fatty acid esters and higher alcohols and components usually blended in the aforementioned external preparations, if necessary.
[0033]
Examples of the support for the plaster agent include a resin film such as a cellulose derivative film, a polyethylene terephthalate film, a nylon film, a polyvinyl chloride film, a polyethylene film, a polyurethane film, and a polyvinylidene chloride film, a metal sheet such as aluminum, a nonwoven fabric, and a woven fabric. A cloth or the like is used, and the resin film and the metal sheet can be used alone or laminated with a nonwoven fabric or the like.
[0034]
For example, in the preparation of an anti-inflammatory analgesic patch provided by the present invention, for example, in an aqueous poultice, benzocaine, a component having an anti-irritating effect, and optionally various components are mixed well and prepared, for example, as a paste. This is coated and laminated with a desired thickness on a support (base material) such as paper, woven fabric, non-woven fabric, or plastic film, and further coated with a transparent protective film such as a polyethylene film. It can manufacture by cutting to the magnitude | size of. The weight of the layer laminated on the base sheet as the drug-containing plaster layer cannot be generally limited, but the coating amount is 200 to 2000 g / m 2 , preferably 400 to 1500 g / m 2 .
[0035]
In the case of plaster agents, for example, synthetic rubber adhesives such as styrene-isoprene-styrene block copolymers, softeners, tackifiers, antioxidants and fillers are melt-kneaded, and benzocaine, A component having an irritating effect and various components as desired may be added and kneaded uniformly, and then spread on a support film and cut into an appropriate size and shape.
【Example】
The anti-inflammatory analgesic patch of the present invention will be specifically described below by showing Examples and Comparative Examples, but the present invention is not limited to these.
[0036]
Examples 1-3: Aqueous poultice preparation An aqueous poultice base composition having the composition shown in Table 1 below was prepared according to a conventional method, and this was applied to a uniform thickness on a nonwoven fabric, and the surface thereof was covered with a polyethylene terephthalate film. The aqueous poultices of Examples 1 to 3 were obtained.
[0037]
[Table 1]
Table 1: Example formulation examples
Figure 0004596751
[0038]
Comparative Examples 1-3:
An aqueous papp base having the composition shown in Table 2 below (not containing benzocaine) was prepared according to a conventional method, applied to a non-woven fabric to a uniform thickness, and the surface thereof was covered with a polyethylene terephthalate film. 1 to 3 aqueous poultices were obtained.
[0039]
[Table 2]
Table 2: Comparative Example Formulation Example
Figure 0004596751
[0040]
Example 4: Plaster agent According to the following formulation, styrene / isoprene / styrene block copolymer, alicyclic saturated hydrocarbon resin, synthetic rubber and dibutylhydroxytoluene were melt-kneaded, nonyl acid vanillylamide, methyl salicylate, dl -After adding camphor and benzocaine and kneading uniformly, it spread | deployed on the support body film and obtained the plaster agent.
[0041]
Formula:
Nonyl acid vanillylamide 0.01% by weight
Methyl salicylate 5.0% by weight
dl-Camphor 2.0% by weight
Benzocaine 5.0% by weight
Styrene / isoprene / styrene block copolymer 22.0% by weight
Alicyclic saturated hydrocarbon resin 46.99% by weight
Synthetic rubber 18.0% by weight
Dibutylhydroxytoluene 1.0% by weight
[0042]
Test Example 1:
The aqueous cataplasm of Examples 1 to 3 and Comparative Examples 1 to 3 and the plaster of Example 4 were affixed to the inner side of the upper arm of 20 subjects and stimulated 10, 20, 30, 60 and 90 minutes after application. Was evaluated by a sensory test.
The evaluation criteria for the stimulus were divided into the following five stages and indicated by the average value of 10 subjects.
4: Strong pain 3: Feeling pain in addition to stimulation 2: Feeling moderate stimulation 1: Feeling weak stimulation 0: Not feeling stimulation The results are shown in Table 3.
[0043]
[Table 3]
Table 3: Irritation test results
Figure 0004596751
[0044]
As can be seen from the results shown in Table 3 above, the patches of the present invention (Examples 1 to 4) exhibited moderate irritation in about 20 minutes after application, and 30 to 90 compared to the comparative examples. In the sticking time of minutes, the pain to the stimulus was rarely felt, and the moderate stimulus was sustained.
[0045]
Test example 2:
The patch of Example 1 and Comparative Example 1 was used for 10 in-house volunteers with symptoms of joint pain (under the supervision of a doctor, informed consent was obtained) and the effects were evaluated.
The evaluation criteria are as follows.
++: Pain was reduced and eased +: Pain was reduced a little ±: No change-: Pain increased The results are shown in Table 4.
[0046]
[Table 4]
Table 4: Effect test results
Figure 0004596751
[0047]
Test Example 3:
The patches of Example 3 and Comparative Example 3 were used for 10 in-house volunteers (under the supervision of doctors, obtaining informed consent) with the symptoms of low back pain, and their effects were evaluated.
The evaluation criteria are as follows.
++: Pain was reduced and eased +: Pain was reduced a little ±: No change-: Pain increased The results are shown in Table 5.
[0048]
[Table 5]
Table 5: Effect test results
Figure 0004596751
[0049]
As can be seen from the results shown in Tables 4 and 5 above, the patch of the present invention has a higher efficacy rate for the symptoms of joint pain or back pain than the patch of the comparative example. It was.
[0050]
【The invention's effect】
As described above, the patch of the present invention is a combination of benzocaine and a component having counter-irritation effect as an active ingredient, compared with a conventional formulation having a component having counter-irritant effect. In addition, it has a skin irritation mitigating effect, and also exhibits the expected anti-inflammatory analgesic effect sufficiently.
Therefore, its medical effect is enormous.

Claims (2)

水分を１０〜８０重量％含有する水性パップ膏体中に、ベンゾカインを０．５〜２０重量％配合し、さらにｌ−メントール、ｄｌ−メントール、ｄｌ−カンフル、ｄ−カンフル、サリチル酸メチル、サリチル酸グリコール、ハッカ油、ユーカリ油、カプサイシン、トウガラシ抽出物、ノニル酸ワニリルアミドからなる群から選択される反対刺激効果（Counter-irritation）を有する成分を一種または二種以上配合したことを特徴とする消炎鎮痛貼付剤。 Benzocaine is blended in an aqueous pap paste containing 10 to 80% by weight of water, and 0.5 to 20% by weight of benzocaine, and 1-menthol, dl-menthol, dl-camphor, d-camphor, methyl salicylate, glycol salicylate Anti-inflammatory analgesic, characterized by combining one or more ingredients with counter-irritation selected from the group consisting of mint oil, eucalyptus oil, capsaicin, capsicum extract, nonylic acid vanillylamide Agent. 反対刺激効果を有する成分の配合量が、ｌ−メントール、ｄｌ−メントール、ｄｌ−カンフル、ｄ−カンフル、サリチル酸メチル、サリチル酸グリコール、ハッカ油またはユーカリ油にあっては０．０１〜３０重量％、カプサイシン、トウガラシ抽出物またはノニル酸ワニリルアミドにあっては０．００１〜５重量％である請求項１に記載の消炎鎮痛貼付剤。In the case of 1-menthol, dl-menthol, dl-camphor, d-camphor, methyl salicylate, glycol salicylate, mint oil or eucalyptus oil, the blending amount of the component having the counter stimulating effect is 0.01 to 30% by weight, The anti-inflammatory analgesic patch according to claim 1 , which is 0.001 to 5% by weight in capsaicin, capsicum extract or nonylic acid vanillylamide.
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JP2003166774A JP4596751B2 (en) 2003-06-11 2003-06-11 Anti-inflammatory analgesic patch
AU2004246924A AU2004246924B2 (en) 2003-06-11 2004-06-10 Anti-inflammatory analgesic adhesive patch
KR1020057020411A KR100946605B1 (en) 2003-06-11 2004-06-10 Anti-inflammatory analgesic adhesive patch
TW093116629A TWI348383B (en) 2003-06-11 2004-06-10 Anti-inflammation pain-relieved patch
EP04745727A EP1632226A4 (en) 2003-06-11 2004-06-10 Anti-inflammatory analgesic adhesive patch
CNA2004800164330A CN1805739A (en) 2003-06-11 2004-06-10 Anti-inflammatory analgesic adhesive patch
CA2528649A CA2528649C (en) 2003-06-11 2004-06-10 Analgesic and anti-inflammatory patch
US10/560,471 US20070207088A1 (en) 2003-06-11 2004-06-10 Anti-Inflammatory Analgesic Adhesive Patch
PCT/JP2004/008097 WO2004110428A1 (en) 2003-06-11 2004-06-10 Anti-inflammatory analgesic adhesive patch

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Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006206471A (en) * 2005-01-26 2006-08-10 Nitto Denko Corp Tape preparation
DE102006060439A1 (en) 2006-12-19 2008-06-26 Henkel Kgaa Cosmetic or dermatological composition for treating e.g. cellulite contains hyperemisating active ingredients and active ingredients for reducing the degranulation of mast cells and/or for releasing histamine
US20100215721A1 (en) * 2007-05-17 2010-08-26 Kenichi Noguchi Poultice and process for producing the poultice
US20110020440A1 (en) * 2007-11-19 2011-01-27 Cadila Pharmaceuticals Limited Stable solutions of sparingly soluble actives
MX2010008456A (en) * 2008-01-31 2010-08-30 Hisamitsu Pharmaceutical Co Adhesive patch.
EP2098254A1 (en) 2008-03-06 2009-09-09 Bayer MaterialScience AG Medical adhesives for surgery with bioactive compounds
ES2425356T3 (en) * 2008-04-15 2013-10-14 Firmenich S.A. Sensory warmth composition
KR100976548B1 (en) 2008-09-12 2010-08-17 김희구 pad for herb remedy and method for manufacturing thereof
WO2011031116A2 (en) * 2009-09-14 2011-03-17 Kim Hee Gu Pad for herbal medicine in which release of medicinal ingredient can be controlled, and manufacturing method thereof
US10980752B2 (en) 2009-09-14 2021-04-20 Bm Biotechnology Co., Ltd. Device for herbal medicine in which release of medicinal ingredient can be controlled, and manufacturing method thereof
CN101961418B (en) * 2010-08-17 2012-08-08 浙江省医学科学院 Double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch
US8900646B2 (en) * 2012-01-05 2014-12-02 Danny Justman Composition and method for minimizing bulling behavior of cattle
US20160128950A1 (en) * 2013-06-28 2016-05-12 Sumair Mitroo Tape having transdermal analgesic properties
MA41266A (en) * 2014-12-22 2017-10-31 Hisamitsu Pharmaceutical Co POULTICE
CN106073982A (en) * 2016-06-16 2016-11-09 广州仁益医疗器械有限公司 Scrotum Medical cooling pastes
US20200375915A1 (en) * 2017-04-25 2020-12-03 Srinivas Reddy Male Matrix adhesive patch and process for the preparation thereof
KR101882679B1 (en) * 2017-08-11 2018-07-27 이태완 Low Irritating of Transdermal Drug Delivery System for Anti-inflammatory and its Manufacturing Method
CN111655248B (en) * 2018-01-24 2023-05-05 久光制药株式会社 Adhesive agent

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4997853A (en) * 1988-12-02 1991-03-05 Galenpharma, Inc. Method and compositions utilizing capsaicin as an external analgesic
JPH06145049A (en) * 1992-11-02 1994-05-24 Taisho Pharmaceut Co Ltd Cross-linking type cataplasm base
JPH08225443A (en) * 1994-12-19 1996-09-03 Taisho Pharmaceut Co Ltd Plaster for poultice
JPH1135475A (en) * 1997-07-18 1999-02-09 Teikoku Seiyaku Co Ltd Preparation containing roripa nasturtium-aquaticum extract and used for external use
JP2001240535A (en) * 1999-10-20 2001-09-04 Toko Yakuhin Kogyo Kk Cool cataplasm
JP2002119529A (en) * 2000-10-19 2002-04-23 Toko Yakuhin Kogyo Kk Base material for cooling patch
JP2003095985A (en) * 2001-09-26 2003-04-03 Lion Corp Blood circulation-promotive composition

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4855294A (en) * 1988-09-06 1989-08-08 Theratech, Inc. Method for reducing skin irritation associated with drug/penetration enhancer compositions
US5859066A (en) * 1996-04-08 1999-01-12 Rutgers, The State University Of New Jersey Method for the treatment of itching
US5885597A (en) * 1997-10-01 1999-03-23 Medical Research Industries,Inc. Topical composition for the relief of pain
US6471984B1 (en) * 1998-01-14 2002-10-29 Hisamitsu Pharmaceutical Co., Inc. Cataplasm and tape-aid containing a plasticizer
US6120792A (en) * 1998-04-29 2000-09-19 Juni; Jack E. Medicated skin patch and method for its use
DE19833177A1 (en) * 1998-07-23 2000-01-27 Labtec Gmbh Rapidly acting plaster preparation for treating irritation due to nettle stings or insect bites, preferably containing menthol and benzocaine
US6284797B1 (en) * 1999-04-12 2001-09-04 Donald A. Rhodes Topical treatment of pain and to promote healing
EP1170020A4 (en) * 1999-12-27 2009-05-06 Teikoku Seiyaku Kk Patches for external use
US6902739B2 (en) * 2001-07-23 2005-06-07 Nutracea Methods for treating joint inflammation, pain, and loss of mobility
US20030118655A1 (en) * 2001-12-21 2003-06-26 Nikhil Kundel Film forming liquid composition
JP2003250829A (en) * 2001-12-27 2003-09-09 Lion Corp External remedy composition
JP2003335663A (en) * 2002-05-20 2003-11-25 Medorekkusu:Kk Antiinflammatory and analgesic preparation for external use
JP2004123632A (en) * 2002-10-03 2004-04-22 Medorekkusu:Kk Anti-inflammatory and analgesic preparation for external use
US20040191302A1 (en) * 2003-03-28 2004-09-30 Davidson Robert S. Method and apparatus for minimizing heat, moisture, and shear damage to medicants and other compositions during incorporation of same with edible films
US6865912B2 (en) * 2002-12-27 2005-03-15 Lg Electronics Inc. Washing machine

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4997853A (en) * 1988-12-02 1991-03-05 Galenpharma, Inc. Method and compositions utilizing capsaicin as an external analgesic
JPH06145049A (en) * 1992-11-02 1994-05-24 Taisho Pharmaceut Co Ltd Cross-linking type cataplasm base
JPH08225443A (en) * 1994-12-19 1996-09-03 Taisho Pharmaceut Co Ltd Plaster for poultice
JPH1135475A (en) * 1997-07-18 1999-02-09 Teikoku Seiyaku Co Ltd Preparation containing roripa nasturtium-aquaticum extract and used for external use
JP2001240535A (en) * 1999-10-20 2001-09-04 Toko Yakuhin Kogyo Kk Cool cataplasm
JP2002119529A (en) * 2000-10-19 2002-04-23 Toko Yakuhin Kogyo Kk Base material for cooling patch
JP2003095985A (en) * 2001-09-26 2003-04-03 Lion Corp Blood circulation-promotive composition

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